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Derm Pharm 2020 > 1 - SYSTEMIC RETINOIDS > Flashcards

1 - SYSTEMIC RETINOIDS Flashcards

1
Q

Tretinoin (Retrieve cream) is all-trans-retinoic acid

A

True

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2
Q

Isotretinoin is 13-cis retinoic acid

A

True

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3
Q

Isotretinoin (13-cis retinoic acid) and tretinoin (all-trans-retinoic acid) are first generation retinoids (non-aromatic retinoids)

A

True

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4
Q

Acitretin is a second generation retinoid (monoaromatic retinoids)

A

True

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5
Q

Acitretin is an acid metabolite of another second generation retinoid etretinate (phased out due to prolonged presence in subcutaneous fat)

A

True

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6
Q

Topical Tazarotene, topical Adapalene, Bexarotene are third generation retinoids (polyaromatic retinoids)

A

True

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7
Q

Tretinoin, Isotretinoin (both first generation retinoids), Acitretin (second generation retinoid) and bexarotene (third generation retinoid) are bound to plasma proteins with the former 3 bound specifically to albumin

A

True

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8
Q

All retinoids are metabolised in the liver by CYP3A4

A

True

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9
Q

Acitretin has a higher bioavailability than Isotretinoin

A

True (60% vs 25%)

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10
Q

Tretinoin, Isotretinoin and Acitretin are excreted in the bile (faeces) and urine

A

True

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11
Q

Bexarotene is excreted in the bile and urine

A

False (only hepatobiliary)

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12
Q

Retinoids are vitamin A derivatives

A

True

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13
Q

Vitamin A can be synthesised in vivo

A

False (must be acquired through the diet)

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14
Q

Beta-carotene (a carotenoid) is a precursor of vitamin A and is converted to retinal (vitamin A aldehyde)

A

True

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15
Q

Retinal (vitamin A aldehyde) the 11-cis isomer and 11-trans isomer is important in the biochemical reaction of visual function

A

True

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16
Q

Retinol (vitamin A alcohol) is essential to reproduction

A

True

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17
Q

Retinol (vitamin A alcohol) and retinal (vitamin A aldehyde) can be converted interchangeably

A

True

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18
Q

Retinol (vitamin A alcohol) is irreversibly metabolised to retinoic acid

A

True

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19
Q

Retinal (vitamin A aldehyde) and retinoic acid play an essential role in epithelial differentiation and normal growth

A

True

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20
Q

Third generation retinoids are more potent than earlier generation retinoids and their therapeutic index (efficacy:toxicity ratio) shows no signs of improvement due to increased toxicity

A

True

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21
Q

The oral bioavailability of retinoids is reduced with food intake

A

False (enhanced with food intake especially fatty food)

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22
Q

Isotretinoin, Acitretin and Bexarotene are relatively water soluble

A

True (Isotretinoin and Acitretin undetectable in serum within 1 month after stopping therapy)

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23
Q

The hepatic metabolism of retinoids is induced mainly by retinoids themselves but also by other agents known to induce hepatic CYP3A4

A

True

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24
Q

Tretinoin has the shortest half life

A

True (tretinoin - bexarotene - Isotretinoin - Acitretin)

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25
Q

Acitretin has the longest half life

A

True (tretinoin - bexarotene - Isotretinoin - Acitretin)

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26
Q

Acitretin (50 hours) has a longer half life than Isotretinoin (10-20 hours)

A

True (tretinoin - bexarotene - Isotretinoin - Acitretin)

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27
Q

Isotretinoin (10-20 hours) has a longer half life than bexarotene (7-9 hours)

A

True (tretinoin - bexarotene - Isotretinoin - Acitretin)

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28
Q

Alcohol indirectly enhances the re-esterification of Acitretin to Etretinate (lipophilic second generation retinoid that preceded its acid metabolite Acitretin which is stored and slowly released from adipose tissue resulting in a prolonged half life of 2.9 years)

A

True (this re-esterification is the reason why contraception for 3 years after cessation of Acitretin is recommended in women of child bearing age)

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29
Q

Retinoids are small molecule hormones that elicit their biological effects by activating nuclear receptors and regulating gene transcription

A

True

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30
Q

Retinoids exert their physiologic effects by binding to receptors present in the nucleus

A

True

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31
Q

There are 2 families of retinoid receptors - retinoic acid receptor (RAR) family and retinoid X receptor (RXR) family

A

True

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32
Q

The retinoic acid receptor (RAR) family has 3 Isoforms - alpha, beta and gamma

A

True (same as RXR)

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33
Q

The retinoid X receptor (RXR) family has 3 Isoforms - alpha, beta and gamma

A

True (same as RAR)

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34
Q

Retinoic acid receptors (RAR) are always and exclusively paired with Retinoid X receptors (RXR)

A

True

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35
Q

Retinoid X receptor (RXR) can exist as a homodimer with another retinoid X receptor (RXR)

A

True (whereas RAR needs to be paired with an RXR)

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36
Q

Retinoid X receptor (RXR) may be paired with another RXR, a Retinoic acid receptor (RAR), vitamin-D3 receptor, thyroid hormone receptor, and peroxisome proliferator-activated receptor

A

True

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37
Q

There are a total of 6 Isoforms of retinoid receptors - RAR alpha, beta, gamma and RXR alpha, beta, gamma receptors

A

True

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38
Q

Retinoid receptors are part of a large superfamily of receptors consisting also of glucocorticosteroid, thyroid hormone and vitamin-D3 receptors

A

True

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39
Q

Acitretin (second generation retinoid) has a weak interaction with multiple Retinoid Acid Receptors (RAR) by activating these receptors but not binding to them

A

True

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40
Q

Alitretinoin (third generation retinoid) is a pan-retinoid receptor and binds to all 6 known retinoid receptors (RAR alpha, beta, gamma and RXR alpha, beta, gamma)

A

True

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41
Q

Tretinoin (First generation retinoid) binds to RAR

A

True

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42
Q

Isotretinoin (First generation retinoid) has no clearly identified affinity for any retinoid receptor (RAR or RXR)

A

True

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43
Q

There is a higher affinity for RXR than RAR with the higher generation retinoids

A

True (third generation Retinoids Alitretinoin and Bexarotene have a higher affinity for RXR)

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44
Q

Topical retinoids Adapalene and Tazarotene (third generation retinoids) binds to RAR beta and gamma Isoforms

A

True (in contrast to the other systemic and topical third generation retinoid Bexarotene which has an affinity for RXR instead of RAR)

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45
Q

Systemic retinoids affect the pathways involved in inflammation

A

True

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46
Q

Systemic retinoids affect the pathways involved in cellular differentiation

A

True

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47
Q

Systemic retinoids affect the pathways involved in apoptosis

48
Q

Systemic retinoids affect the pathways involved in sebaceous gland activity

49
Q

Patients on systemic retinoids may concomitantly take vitamin A supplementation as long as this is < 5000 IU daily

50
Q

Oral administration of retinoids with milk or fatty foods reduces retinoid absorption

A

False (enhances retinoid absorption, though patients should avoid excessively fatty diet)

51
Q

Women with childbearing potential must not consume alcohol during and up to 2 months after cessation of Acitretin therapy

A

True (alcohol enhances the re-esterification of Acitretin to Etretinate which is more lipophilic and able to be stored in tissue and slowly released for up to 2.9 years)

52
Q

In males and females of non-child bearing potential, the consumption of alcohol with the risk of re-esterification of Acitretin to Etretinate is not a clinically important issue

53
Q

Isotretinoin (First generation retinoid) is FDA approved for acne vulgaris

54
Q

Acitretin (second generation retinoid) is FDA approved for psoriasis

55
Q

Bexarotene (third generation retinoid) is FDA approved for selected cases of mycosis fungoides and Sezary syndrome

56
Q

The initial clinical effects of Acitretin in psoriasis are often seen in 4-6 weeks but it may take up to 3-4 months or longer to see the full clinical benefit

57
Q

Combination therapy with systemic retinoids (Acitretin) and phototherapy for psoriasis is more effective than monotherapy with either modality

58
Q

Current recommendations for combination Acitretin and UV therapy for psoriasis include instituting low dose (25mg) Acitretin 2 weeks prior to the initiation of phototherapy

59
Q

If combination Acitretin and UV therapy is used in psoriasis, the UV dose should be adjusted downward to accommodate the Acitretin effect

60
Q

Acitretin can be used in combination with methotrexate, however every attempt should be made to limit the period for which patients are taking both medications due to the potential adverse liver effects

61
Q

Acitretin can be used in combination with CsA, however every attempt should be made to limit the period for which patients are taking both medications due to the possible elevations in serum triglycerides

62
Q

Retinoids are immunosuppressive

A

False (generally not considered to be immunosuppressive and so may be ideal candidates for combination therapy with biological agents)

63
Q

Patients taking Isotretinoin for acne vulgaris may expect that their complexion may worsen for the first 4-6 weeks of Isotretinoin therapy

64
Q

Retinoids are teratogenic

65
Q

Effective contraception or abstinence should commence 1 month prior to starting Isotretinoin and Acitretin therapy

66
Q

Effective contraception must be continued 1 month after discontinuation of Isotretinoin therapy

67
Q

Effective contraception must be continued 3 years following the discontinuation of Acitretin due to the re-esterification to etretinate with concomitant alcohol use

A

True (etretinate has an exceptionally long elimination half life)

68
Q

It is not clear what quantity of ingested alcohol is required for the re-esterification of Acitretin to Etretinate

69
Q

There is a risk of retinoid embryopathy in fetuses fathered by men taking systemic retinoids

A

False (there is little, if any risk)

70
Q

Patients should have 2 negative urine or serum pregnancy tests before receiving the initial Isotretinoin prescription

71
Q

The second pregnancy test should be done during the first 5 days of the menstrual period immediately preceding the start of Isotretinoin therapy

72
Q

For patients who are amenorrhea, the second pregnancy test should be done at least 11 days after the last unprotected sexual intercourse (without using 2 effective forms of contraception, prior to starting Isotretinoin therapy

73
Q

Each month of Isotretinoin therapy, the patient must have a negative pregnancy test result

74
Q

Patients on Isotretinoin therapy must commit to 2 forms of contraception

75
Q

Hypersensitivity to parabens is a contraindication to Isotretinoin therapy

A

True (Parabens are present in Isotretinoin capsules)

76
Q

Systemic retinoids can cause spontaneous abortion

77
Q

Pancreatitis is a risk of Bexarotene, but also reported with Isotretinoin

78
Q

Dry mucous membranes (cheilitis and nasal mucosa) and skin (xerosis) is common in patients taking Isotretinoin and Acitretin

79
Q

Cutaneous xerosis associated with Isotretinoin and Acitretin is more common in patients with a history of atopy

80
Q

Acitretin may induce ‘sticky skin’ especially on the palms

81
Q

Systemic retinoids may cause an exuberant granulation tissue response in previous acne lesions, around nail folds, and at sites of trauma

82
Q

Acne fulminans can occur with Isotretinoin use

83
Q

Elevated serum lipids, especially triglyceride levels is much greater with Bexarotene than other systemic retinoids

A

True (occurred within the first or second week of therapy)

84
Q

Statins and fenofibrate (fibric acid derivative) can be used as lipid lowering agents in conjunction with Bexarotene

A

True (both lipid lowering agents are not inhibitors of the Cytochrome P450 pathway and so do not affect the metabolism of Bexarotene with the risk of increase Bexarotene and triglyceride levels)

85
Q

Gemfibrozil (also a fibric acid derivative) is contraindicated with Bexarotene as it is a Cytochrome P450 pathway inhibitor which causes an increase of Bexarotene and triglyceride levels

A

True (Bexarotene is metabolised by the Cytochrome P450 pathway in the liver)

86
Q

Lipid elevations associated with systemic retinoid therapy are reversible upon cessation of therapy

87
Q

There is contradictory evidence that Isotretinoin is a cause of depression

88
Q

The data regarding Isotretinoin use as a cause of Inflammatory Bowel Disease is conflicting

89
Q

There is potential for systemic retinoids to cause diffuse interstitial skeletal hyperostosis (DISH), similar bone effects in chronic vitamin A toxicity

A

True (may be asymptomatic risk in Isotretinoin, although true risk is only when systemic retinoids are given in high doses and prolonged period)

90
Q

If diffuse interstitial skeletal hyperostosis (DISH) involves the posterior longitudinal ligament, this may lead to spinal cord compression and neurological deficits and therefore consideration should be given to discontinuing the retinoid

91
Q

Systemic retinoids may cause premature epiphyseal closure

A

True (rare and only occurring in higher doses)

92
Q

Blepharoconjunctivitis has been associated with Isotretinoin and Acitretin

93
Q

Corneal opacities can also occur in patients taking systemic retinoids

A

True (occur in central and peripheral cornea and do not adversely affect vision)

94
Q

Decreased night vision is exclusively associated with Isotretinoin

95
Q

Bacterial conjunctivitis has been associated with Isotretinoin (uncommon)

96
Q

Both Acitretin and Isotretinoin may cause elevated transaminases

97
Q

Elevated transaminases in Isotretinoin use are mild and return to normal despite continued therapy

98
Q

There have been cases of severe hepatitis reported with Acitretin use

99
Q

Elevated transaminases which are more persistent in Acitretin therapy are usually mild and not considered to be clinically significant

A

True (Acitretin should be discontinued for severe (> 3 fold) increase of liver transaminases elevations)

100
Q

Elevated Transaminases as a result of Bexarotene therapy occur less frequently

101
Q

Acitretin is more likely to cause an idiosyncratic fatal hepatitis reaction than the other systemic retinoids

102
Q

Acitretin should be discontinued for severe (> 3 fold) increase of liver transaminases elevations

103
Q

Thyroid effects (Central hypothyroidism) is most commonly reported for Bexarotene

A

True (RXR heterodimers with thyroid receptors)

104
Q

Systemic retinoids may cause pseudotumour cerebri (headaches with nausea, vomiting and visual changes), especially with concomitant tetracycline, doxycycline, and minocycline

105
Q

Muscle effects (myalgias) are associated mostly with Isotretinoin therapy

106
Q

Telogen effluvium is greater with Acitretin than Isotretinoin or Bexarotene

107
Q

Nail fragility may be associated with systemic retinoids

108
Q

The incidence of Nail dystrophy and onycholysis is higher with Acitretin

109
Q

Patients on Bexarotene (third generation retinoid) are at risk of reversible leukopenia and neutropenia

A

True (less frequent with first and second generation retinoids)

110
Q

Systemic retinoids may cause photosensitivity

111
Q

Concomitant Vitamin A supplementation and systemic retinoids may induce hypervitaminosis A-like toxicities

112
Q

CYP3A4 inhibitors I.e. Macrolide antibiotics (erythromycin, clarithromycin, roxithromycin) and Azole antifungals may increase systemic retinoid drug levels and result in potential toxicity

A

True (retinoids are metabolised on the liver by CYP3A4)

113
Q

CYP3A4 Inducers I.e. Antituberculosis drugs (rifampicin) and Anticonvulsants (Phenytoin, carbamazepine) may reduce systemic retinoid drug levels

A

True (retinoids are metabolised on the liver by CYP3A4)

114
Q

Systemic retinoids may increase CsA levels and result in potential toxicity via competition with retinoids for CYP3A4 metabolism

A

True (both retinoids and CsA are CYP3A4 substrates)

115
Q

Retinoids may reduce the drug levels of progestin only contraceptives causing reduced efficacy of these contraceptives

Derm Pharm 2020 (47 decks)

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